Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 311.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.21 mL||16.04 mL||32.08 mL|
|5 mM||0.64 mL||3.21 mL||6.42 mL|
|10 mM||0.32 mL||1.6 mL||3.21 mL|
|50 mM||0.06 mL||0.32 mL||0.64 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Hurst et al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066
Timmermann et al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074
Kalappa et al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819
If you know of a relevant reference for PNU 120596, please let us know.
View Related Products by Product Action
Keywords: PNU 120596, supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, active, vivo, Nicotinic, Receptors, Acetylcholine, PNU120596, Nicotinic, (a7), Receptors, Tocris Bioscience
8 Citations for PNU 120596
Citations are publications that use Tocris products. Selected citations for PNU 120596 include:
Yamauchi et al (2012) Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. Nat Commun 82 687 PMID: 22784805
Kasheverov et al (2015) 6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor. Mar Drugs 13 1255 PMID: 25775422
Thomsen et al (2015) α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties. PLoS One 10 e0130572 PMID: 26086615
John et al (2015) Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. PLoS One 1601 15 PMID: 25553616
Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. PLoS One 10 e0125116 PMID: 25906356
Zhang et al (2015) Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor. Mol Pharmacol 10 e0137588 PMID: 26340537
daCosta et al (2015) Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors. J Neurosci 6 8057 PMID: 26282895
Maldifassi et al (2014) A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages. PLoS One 9 e108397 PMID: 25259522
Do you know of a great paper that uses PNU 120596 from Tocris? If so please let us know.
Literature in this Area
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.